公开(公告)号：US20030171440A1

公开(公告)日：2003-09-11

申请号：US10308878

申请日：2002-12-02

Applicant: SEPRACOR INC.

Inventor： Chris Hugh Senanayake ,  Thomas P. Jerussi ,  Paul T. Grover ,  Qun Kevin Fang ,  Mark Currie

IPC: A61K031/137 ,  A61K031/704 ,  A61K031/277 ,  C07D211/22 ,  A61K031/445 ,  A61K031/40

CPC classification number: C07C217/74 ,  C07C217/52 ,  C07C255/59 ,  C07C2601/02 ,  C07C2601/14

Abstract: Compounds of formula I are effective in treating disorders modulated by opiate receptor activity and/or monoamine activity. 1 In formula I, R1 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl; R2 is selected from hydrogen, hydroxy, cyano, haloalkyl, glycosyl, SO2R5, and OR5; R3 and R4 are independently selected from hydrogen and lower alkyl, or R3 and R4 taken together with nitrogen form a five- or six-membered heterocyclic or substituted heterocyclic ring; and R5 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl.

Abstract translation: 式I的化合物在治疗由阿片剂受体活性和/或单胺活性调节的病症中是有效的。 在式I中，R 1选自烷基，芳基，烷基芳基，取代的烷基，取代的芳基和取代的烷基芳基; R 2选自氢，羟基，氰基，卤代烷基，糖基，SO 2 R 5和OR 5; R 3和R 4独立地选自氢和低级烷基，或R 3和R 4与氮一起形成五元或六元杂环或取代的杂环; R 5选自烷基，芳基，烷基芳基，取代的烷基，取代的芳基和取代的烷基芳基。

公开(公告)号：US20040092605A1

公开(公告)日：2004-05-13

申请号：US10663173

申请日：2003-09-16

Applicant: Sepracor, Inc.

Inventor： Thomas P. Jerussi ,  Qun Kevin Fang ,  Mark G. Currie

IPC: A61K031/135 ,  C07C211/42

CPC classification number: C07C211/42 ,  C07B2200/07 ,  C07C2602/10 ,  C07C2602/28

Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-null4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-ylnullformamide, which are also useful.

Abstract translation: 用（1R，4S） - 反式-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺处理CNS病症; 和（1S，4R） - 反式-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺。 还公开了制备4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺的方法。 该方法包括制备N- [4-（3,4-二氯苯基）-1,2,3,4-四氢萘-1-基]甲酰胺的全部四种异构体，它们也是有用的。

公开(公告)号：US20040087661A1

公开(公告)日：2004-05-06

申请号：US10662997

申请日：2003-09-16

Applicant: Sepracor, Inc.

Inventor： Thomas P. Jerussi ,  Qun Kevin Fang ,  Mark G. Currie

IPC: A61K031/135

CPC classification number: C07C211/42 ,  A61K31/135 ,  A61K45/06 ,  C07C209/50 ,  C07C231/12 ,  C07C313/06 ,  C07C2601/14 ,  C07C2602/10 ,  C07C233/14

Abstract: Treatment of central nervous system disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine and with (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine is also disclosed.

Abstract translation: 用（1R，4S） - 反式-4-（3,4-二氯苯基）-1,2,3,4-四氢-N-甲基-1-萘胺处理中枢神经系统疾病，用（1S，4R） 披露了4-（3,4-二氯苯基）-1,2,3,4-四氢-N-甲基-1-萘胺。 还公开了制备4-（3,4-二氯苯基）-1,2,3,4-四氢-N-甲基-1-萘胺的方法。

公开(公告)号：US20020183281A1

公开(公告)日：2002-12-05

申请号：US10160033

申请日：2002-06-04

Applicant: Sepracor Inc.

Inventor： Chrisantha Hugh Senanayake ,  Qun Kevin Fang ,  Zhengxu Han ,  Dhileepkumar Krishnamurthy

IPC: C08B037/16 ,  C07C249/02 ,  A61K031/724 ,  A61K031/13

CPC classification number: C07C251/18 ,  A61K31/11 ,  A61K31/135 ,  A61K45/06 ,  C07B2200/07 ,  C07C45/44 ,  C07C47/457 ,  C07C211/29 ,  C07C2601/04 ,  A61K2300/00 ,  A61K31/137

Abstract: Methods of making and using racemic and optically pure metabolites of sibutramine, and pharmaceutically acceptable salts, solvates, and clathrates thereof, are disclosed. Pharmaceutical compositions and dosage forms are also disclosed which comprise a dopamine reuptake inhibitor, such as a racemic or optically pure sibutramine metabolite, and optionally an additional pharmacologically active compound.

Abstract translation: 公开了制备和使用西布曲明的外消旋和光学纯的代谢物及其药学上可接受的盐，溶剂合物和笼形物的方法。 还公开了药物组合物和剂型，其包含多巴胺再摄取抑制剂，例如外消旋或光学纯的西布曲明代谢物，以及任选的另外的药理活性化合物。